性质
| Related Categories | Excitatory Amino Acids, Ion Channels, Ionotropic Glutamate Receptor Modulators, Ligand-Gated Ion Channels, NMDA Antagonists, |
| InChI Key | QLTXKCWMEZIHBJ-PJGJYSAQSA-N |
| form | powder |
| optical activity | [α]25/D +117°, c = 1 in methanol(lit.) |
| color | white |
| solubility | DMSO: >20 mg/mL |
| H2O: 6 mg/mL | |
| 0.1 M HCl: soluble |
25 mg in poly bottle
5 mg in glass bottle
50, 250 mg in glass bottle
(+)-MK-801 hydrogen maleate has been used in following experimental studies:
It is injected to mice to study the effect of systemic administration of CIQ [(3-chlorophenyl) (6, 7-dimethoxy-1-((4-methoxyphenoxy) methyl)-3, 4-dihydroisoquinolin-2(1H)-yl)methanone] on schizophrenia-like behaviours stimulated by MK-801.[5]
It has been used to block the NMDA (N-methyl-D-aspartate) receptor-mediated rtPA (recombinant tissue plasminogen activator)-enhanced excitotoxic pathway.[6]
It is injected in varied doses to study behavioral performance altering effects of MK-801 in zebrafish (Danio rerio).[8]
It is used as a NMDA receptor antagonist to study 3-OH-GA-induced neuronal damage via NMDA receptors.[7]
Highly potent and selective non-competitive NMDA glutamate receptor antagonist that acts at the NMDA receptor-operated ion channel as an open channel blocker. Inhibits behavioral sensitization to psychostimulants and ethanol.
MK-801 [(+)-5-methyl-10, 11-dihydroxy-5H-dibenzo (a, d) cyclohepten-5, 10-imine] functions as a selective non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist and stimulates locomotion in monoamine-depleted mice.[2] Experimental study shows that MK-801, influence circling behavior in a direction-specific manner, modify swimming activity and place preference in zebrafish.[3] Acute injection of MK-801, dose dependently, enhances extracellular acetylcholine (ACh) release in the rat parietal cortex.[4] For intracerebral hematomas, MK-801 might act as a potent supplement to reduce delayed edema after recombinant tissue plasminogen activator (rtPA) clot lysis.[6] MK-801 functions as an antidepressant in the social defeat stress model, but it doesn’t have long-lasting effect.[9]
This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®1280), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.
MK-801 [(+)-5-methyl-10,11-dihydroxy-5H-dibenzo(a,d)cyclohepten-5,10-imine] also known as dizocilpine hydrogen maleate is an effective anticonvulsant with both anxiolytic and sympathomimetic properties.[1]
LOPAC is a registered trademark of Sigma-Aldrich Co. LLC
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